Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
210.159294606
InChI
InChI=1S/C9H18N6/c1-13(2)7-10-8(14(3)4)12-9(11-7)15(5)6/h1-6H3
InChI Key
InChIKey=UUVWYPNAQBNQJQ-UHFFFAOYSA-N
IUPAC Name
2-N,2-N,4-N,4-N,6-N,6-N-hexamethyl-1,3,5-triazine-2,4,6-triamine
Traditional IUPAC Name
altretamine
SMILES
CN(C)C1=NC(=NC(=N1)N(C)C)N(C)C
Độ hòa tan
91 mg/L (at 25 °C)
pKa (Strongest Basic)
7.75
Refractivity
65.65 m3·mol-1
Dược Lực Học :
Altretamine is a novel antineoplastic agent. The precise mechanism by which altretamine exerts its cytotoxic effect is unknown, although a number of theoretical possibilities have been studied. Structurally, altretamine resembles the alkylating agent triethylenemelamine, yet in vitro tests for alkylating activity of altretamine and its metabolitics have been negative. Altretamine has been demonstrated to be efficacious for certain ovarian tumors resistant to classical alkylating agents. Metabolism of altretamine is a requirement of cytotoxicity. Synthetic monohydroxymethylmelamines, and products of altretamine metabolism, in vitro and in vivo, can form covalent adducts with tissue macromolecules including DNA, but the relevance of these reactions to antitumor activity is unknown.
Cơ Chế Tác Dụng :
An alkylating agent proposed as an antineoplastic. It also acts as a chemosterilant for male houseflies and other insects. [PubChem]
The precise mechanism by which altretamine exerts its cytotoxic effect is unknown although it is classified as an alkylating anti-neoplastic agent. Through this mechanism, the drug is metabolized into alkylating agents by N-demethylation. These alkylating species consequently damage tumor cells.
Dược Động Học :
▧ Protein binding :
94%
▧ Route of Elimination :
Human urinary metabolites were Ndemethylated homologues of altretamine with <1% unmetabolized altretamine excreted at 24 hours.
▧ Half Life :
4.7-10.2 hours
Chỉ Định :
For use as a single agent in the palliative treatment of patients with persistent or recurrent ovarian cancer following first-line therapy with a cisplatin and/or alkylating agent-based combination.
Liều Lượng & Cách Dùng :
Capsule - Oral
Tài Liệu Tham Khảo Thêm
National Drug Code Directory